Vitamin preparation for parenteral administration



\ Patented Feb. 9,

- VITAMIN PREPARATION FOR PARENTERAL ADMINISTRATION Hermann Vollmer,'NewYork, N. Y.

No Drawing. Application. April 2-1, 1941,

Serial No. 339,504

15 Claims.

My present invention relates to a new medicine for parenteraladministration and to a new composition of matter to be used as thismedicine. Herein, the term parenteral administration" is used'asreferring to subcutaneous and intramuscular injections.

This application is a continuation in part of my copending applicationSerial 297,107, filed September 29, 1939 for Vitamin preparation forparenteral administration.

It has been found that vitamin injections administered in oily solutionare slowly adsorbed,

whereas in most cases a quick adsorption and actionisdesired. The speedof absorption of vitamin in oily solution which is injectedintramuscularly'depends chiefly on the extent, of surface contactbetween the oily vehicle and the tissue, and the solubility of thevitamin in the tissue.

It is an object of my present invention" to increase the extent ofsurface contact between the oily vehicle and the tissue. It is a furtherobject of my invention to increase the solubility of the vitamin in thetissue.

In order to increase the surface contact I add to the vitamin in oilysolution a substance adapted to reduce the viscosity of the oilyvehicle. It is further of advantage if the substance added is a bettersolvent for the vitamin administered As a solvent for the abovevitaminsvarious vegetable oils may be used, such for example as peanutoil, olive oil, linseed oil, wheat germ oil, cotton seed oil, rice oiland palm oil. In general, all fatty oils of animal or vegetable originwhich are chemically triglycerides of fatty acids may be used. Iprefer'peanut oil as a carrier and sol-" vent for the vitamin because itis less irritating and causes fewer allergic reactions-than othervegetable oils.

For increasing the surface contact of the oil and reducing the viscositythereof, I propose to incorporate therewith a suitable agentwhich ispreferably also a solvent for the vitamin, for example, ether, pentan,chloroform, aceton, referred, to herein for convenience as ether likesubstances.

The above materials, when used in relatively (oi. lei-a1) This loweringof the viscosity is not in direct ratio to the amount of the substanceused but" follows a hyperbolic curve. Relatively small amounts of theabove substances therefore reduce the viscosity of the oil to a smallfraction of its original value, and the resultant mixture spreadsimmediately after its injection and forms a large contact surface withthe tissues, thereby increasing the interstices of the muscles whichcome in contact "with the vitamin. Since the vitamins are more solublein said ether like substances than in oil, the vitamins are carriedthereby to the cell sterols and fats where the vitamin is absorbed muchmore rapidly than in the case of an oil solution alone.

' for example may remain in situ for many month's without appreciableabsorption.

As a specific example I propose to carry out the administration of thevitamin in a mixture consistingof about 50% to 70% of a vegetable oiland about 50% to 30% or less of a viscosity lowering substance of thetype specified above.

I have found for example that rickets and tetany can be cured byadministration of one single dose of about 600,000 units of vitamin D.

The speed of the curative effect of this shock T therapy depends largelyon the rapidity of ab sorption of the vitamin D administered. ThereforeI propose especially for this therapy the addition of-a substance of theclass referred to above which isadapted' to reduce the viscosity of theoil and is a better solvent.for this massive Certain oils more than500,000 units of'vitaminD, 0.5 to 0.7

cubic-centimeter of vegetable oil, and 0.5 to 0.3

cubic centimeter of ether. Repeated doses of 100,000, units or more mayhowever be used if v This mixture is thin enough to pass throughhypodermic needles. Consequently, the intramuscular injection causeslittle or no pain, an addi-v tional clinical advantage. Probably due tothe germicidalefiect of ether, the solution was found to be sterileWithout sterilization by heat, and

, therefore it may be used without heat sterilization.

small amounts, decrease the viscosity of the oil. Withoutfurtheranalysis, the foregoing so fully reveal the gist oi thisinvention that.others can by'applying current knowledgereadily adapt it rorvariousapplications; 'withoutFomitting certain features, that, irom's'thestandpoint ofthe prior. art," fairly ,constitutei essentialcharacterlstics orthe'pr'esent invention, andtherefore such adaptationsshould and are intended to be comprehended within the mean ing.and rangeof equivalency of the following claims.

What'is claimed is:

1. A therapeutic agent for parenteral admin-. istration comprising, acomposition of matter containing vitamin D, a vegetable loi1,and'ether.

after injection to form rapidly,a large contact surface between thevitamin containing oil and thetissues, or a substance selected from thegroup consisting oi ether, pentan, chloroform and aceton.

9. A therapeutic' agent for parenteral-- administration, comprising avitamin selected from the group consisting of vitaminsA, D, ,E and K,,peanut oil, and an amount, less than 50% and suited to"acce'lerate thespreading of the mixture after injection to form rapidly a large contactin an amount less than 50% and. suitedto ac.-

celerate the spreading of the mixture .afterinJec-.

3. A therapeutic agent for parenteral administration comprising,\ a.composition of: matter consisting of vitaminD in 9, mixture consistingof about 50 to .70 percent or a vegetable oil and about 50 to percent ofether.

. 4.- A therapeutic agent for parenteral administration comprising acomposition of matter consisting of vitamin: D in a mixture consistingof about 50 to'IO percent of peanut oil and about 50 to 30 percent ofether.

5. A therapeutic agent for parenteral administration comprising,acomposition or matter con,

taining in one dose more than 500,000 units of vitamin D, 0.5 to 0.7cubic ;centimeter of a V888:

table oil, and'0.5,to 0.3 cubic centimeter of ether..

'6. A therapeutic agent for parenteral administration comprising, acomposition of matter containing in one dose-about 500,000 unitsot-vitamin 1D,-about 0.6 cubic centimeter of peanut oil, and about 0.4cubic centimeter of ether.

7. A therapeutic agent for parenteral administration comprising acomposition of matter con- 50 tainingdn one dose more than, 100,000units of vitamin D, 0.5 to. 0.7 cubic centimeter of a vegetable oil, and0.5 to 0.3 cubic centimeter of ether.

8.-A therapeutic agent for parenteral 1 administration, comprising avitaminselected from the 56 group consisting of vitamins A, D, E,- and-K, a vegetable oil. and an amount, less than 50% and suited toaccelerate the spreading of the mixture surface between the vitamincontaining oil and the tissues; of (asubstance selected from the group..consisting of ether, p'entan, chloroform and aceton.

10'. A therapeutic agent for parenteral administxation, comprising avitamin selected from the group consisting of vitamins A, D, E and K, avegetableoil, and about 30% to 50% of a substance suited to reduce theviscosity of said oil and selected from the group consisting of ether,pentan, chloroform and aceton. 1151. A therapeutic agent for parenteraladministration, comprising vitamin selected from the group consistingotvitamins A, DE and K, peanut oil, and about 30% to 50% of a substancesuited-to reduce the viscosity .0! said oil and selected from the groupconsisting of, ether, pentan, chloroform and aceton.

12. A-therapeutic agent ,for parenteral administration.- comprising-avitamin selected fropnthe of absorption otthe vitamin by said tissues.

13. A therapeutic agent for parenteral administration, comprising avitamin selected from the group consisting of vitamins A, D, E and K,peanut oil, and ether inan amount less than 50% and suited to acceleratethe spreading of the mixture after injection to form rapidly a largecontact surface between the vitamin containing oil and the tissues,thereby increasing the speed of absorption of'the vitamin by saidtissues.

I 14. A therapeutic agent for parenteral administration, comprising avitamin selected from the group consisting of vitamins A,- D, E and K, avegetable oil and from 30%to 50% of ether.

I 15. A therapeutic agent for parenteral administration, comprising avitamin selected from the group consisting of vitamins A, D, E and K,peanut oil and from 30% to 50% of ether.

HERMANN VOLLMER.

